Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/08—Anti-ageing preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/62—Nymphaeaceae (Water-lily family)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9789—Magnoliopsida [dicotyledons]

Definitions

• the present invention relates to the use of the Lotus plant and especially Lotus extract in oral and topical applications.
• the present invention concerns the addition of methyl donors and other antioxidants to the formulation to protect the body from free radicals, a key factor contributing to aging.
• the human body is assaulted on a daily basis by factors that accelerate the aging process—diet, stress, sun, heat, environment, and the formation of free radicals, which damage the skin cell membrane and DNA by various pathways.
• the free radicals originate from many reactions. For example, molecular oxygen can be stripped of an electron by photons of light (solar radiation), heat, or an oxidant. Thus formed, singlet oxygen is highly reactive and short lived; it quickly adds another electron, producing the super oxide anion radical and the hydroxyl radical. All of these radicals are toxic to cells and highly reactive, causing a cascade of damage that accumulates over the years and contributes to aging.
• free radicals are produced by normal metabolism, where oxygen is used to convert food for energy, as well as in certain diseases, such as infection and inflammation, in which the immune cells use free radicals, such as nitric oxide and superoxide radicals, to destroy bacteria and viruses.
• free radicals if in excess, can produce more damage, in particular to DNA, causing mutations and fragmentations.
• the damage doesn't stop at the cell or molecule that is oxidized, since the oxidized component within the cell or molecule becomes unstable and highly reactive due to its need for an electron, it becomes a free radical attacking other cells or molecules, thereby causing a chain reaction.
• oxidation of lipids and proteins injures cell membranes, weakens blood vessels, modifies enzymes and damages many other molecules. These injuries alter cell functions and increase the risk of heart disease, stroke, and cancers.
• the MT enzyme was present at levels comparable to modern day Sacred Lotus seeds. Damaged proteins did not accumulate within the ancient Sacred Lotus seeds, suggesting that the MT enzyme, possibly along with other constituents, such as methyl donors and antioxidants, kept the ancient Sacred Lotus seeds alive for so many years.
• the present invention alleviates and overcomes certain of the above-mentioned problems and shortcomings of the present state of the art through the discovery of novel acceptable oral and topical delivery systems and compositions for effectively treating and preventing signs of aging, repairing damaged skin and restoring skin to a more youthful appearance and methods of using the same.
• the object of the invention to provide a general method for prevention or alleviation of age-related damage to the skin and associated decline of body function and appearance from aging through the topical and/or internal use of a composition in combination with a suitable carrier or vehicle.
• Another object is to enhance a cosmetic composition to make the skin appear younger by adding Sacred Lotus and methyl donors.
• Another object is to restore the skin to a more youthful appearance.
• Another object is the formulation of dietary supplements to nourish and protect skin from within.
• Another object is to have the person taking the supplement experience improvement in physical attributes helping the person to feel younger and look younger; have increased stamina; have increased sexual function; have improved circulation; have improved hair and nail strength and growth; have improved vision; have improved mental focus, performance and memory; have improved overall health; have improved immune function; have improved body composition, with greater muscle tone; have improved body composition, with less body fat; have improved ability to sleep; have improved vitality; have improved energy; have improved mood; restore skin to a more youthful appearance; improve the vibrancy of skin; improve the smoothness of skin; improve the tone of skin; improve the elasticity of skin; and have less wrinkles.
• Another object is to use additional antioxidants to counter the deleterious effects of free radicals.
• Another object is to add Lotus extract and methyl donors to existing preparations to reduce the appearances of lines and wrinkles.
• Another object is to use the extract of Sacred Lotus ( Nelumbo nucifera ) as a natural source of methyltransferase. It has now been observed, surprisingly and unexpectedly, that by using an extract of Lotus in combination with methyl donors by topical application or oral ingestion, signs of aging can be reduced, eliminated or even reversed.
• Another object of the present invention are formulations of Lotus extract in combination with methyl donors in dermatologicals, such as gels, lotions, powders, tablets, capsules, creams, sunscreens, cleansers, and various skin care formulas to repair the damage from aging, reduce further damage and restore skin to a more youthful appearance.
• dermatologicals such as gels, lotions, powders, tablets, capsules, creams, sunscreens, cleansers, and various skin care formulas to repair the damage from aging, reduce further damage and restore skin to a more youthful appearance.
• the formulation is a suitable cosmetic or dermatologically or orally acceptable non-toxic, non-allergenic carrier containing a variety of components.
• the present invention uses Lotus extract in skin and dietary formulas to combat aging. It is believed that the use of Lotus extract in cosmetics and dietary supplements accomplish anti-aging effects based on anti-aging factors (enzymes such as methyltransferase) which are present in the Lotus plants and seeds.
• anti-aging factors enzyme such as methyltransferase
• Lotus extracts contain certain anti-oxidants such as vitamin C and glutathione which may contribute to anti-aging effects on skin along with methyltransferase and may even contain other beneficial factors.
• methyltransferase and/or the natural compounds found in an extract of Lotus plants may be used in an effort to repair age related signs of the skin such as lines, spots, wrinkles, and/or loss of elasticity.
• Other sources of methyltransferase that may be used in the invention are extracts of Sacred Lotus seeds or other components of the Sacred Lotus plants, extracts of Yellow Lotus seeds or components of Yellow Lotus plants, extracts of Purple Lotus seeds or other components of Purple Lotus plants, extracts of Blue Lotus seeds or other components of Blue Lotus plants, extracts of White Lotus seeds or other components of White Lotus plants, extracts of other Lotus seeds or components of other Lotus plants where methyltransferase may be present, wheat germ oil, liver, brain, other animal parts including glands, and bio-fermentation or chemical synthesis for example.
• An extract is prepared, for example, as follows. Maceration is the preferred process, since no heat is used which may destroy or alter temperature sensitive components; however percolation, digestion, infusion and decoction are within the scope of the invention as more scientific information becomes available.
• a twenty percent extract of Nelumbo nucifera is used and prepared by placing 200 grams of finely milled untreated whole seeds, including husks and piths, in a stoppered container with about 750 mL of a 50/50 wt/wt mixture of purified water and propylene glycol USP and allowed to stand for a period of at least three days in a warm place with frequent agitation, until soluble matter is dissolved. The mixture is filtered and, after most of the liquid has drained, the residue on the filter is washed with sufficient quantity of solvent mixture; the filtrates are combined to produce 1000 mL.
• the present inventor has been experimenting with the use of Lotus seed extract in oral and topical formulations since 1996. Ongoing research has revealed that colorful fruits and vegetables, such as carrots and broccoli, contain excellent antioxidant properties. As evidenced by their names (Blue Lotus, Yellow Lotus, Purple Lotus, etc.), the flowers of the Nelumbo family are also very colorful. The present inventor realized that the pigments contained in the Lotus flower would act similarly to antioxidants and that the combination of Lotus seed extract and Lotus flower extract may prevent free radical damage and extend the youthfulness of the skin.
• Sacred Lotus is a preferred species and the seed and flower are the preferred parts
• other parts of the plant or other species such as the Yellow Lotus ( Nelumbo lutea ), Blue Lotus ( Nelumbo caerulea ), White Lotus or other Lotus varieties containing these anti-aging enzymes or constituents are believed to be suitable alternatives for accomplishing the objectives of the present invention.
• methyltransferase and/or the natural compounds found in the extract of the Lotus is used to combat the natural aging process.
• the skin is also subject to external factors that contribute to accelerating the aging process.
• the present invention combats these external factors utilizing extract of the Lotus in combination with methyl donors. It is believed that this mixture provides added protection from external factors that damage the skin.
• the present invention combines Lotus extract with methyl donors.
• Lotus extract contains the L-isoaspartyl methyltransferase enzyme.
• the methyltransferase enzyme catalyzes the transfer of a methyl group to an acceptor molecule.
• Many different methyltransferase reactions have been documented in the literature, including 1-phenanthrol methyltransferase activity, 5,10-methylenetetrahydrofolate-dependent methyltransferase activity, 5-methyl-5,6,7,8-tetrahydromethanopterin-dependent methyltransferase activity, to name a few.
• the Lotus extract contains the L-isoaspartyl methyltransferase enzyme, which transfers a methyl group to damaged L-isoaspartyl residues. This mechanism serves to repair cell damage to all human cells.
• Methyl donors include any compounds that have a methyl (—CH 3 ) side chain.
• Some suitable examples include methionine, betain (aka trimethylglycine), dimethylglycine, choline, polyenyphosphatidylcholine, phosphatidylserine, phosphatidyl choline (lecithin), glycerylphosphoryl choline, and S-adenosyl-L-methionine (“SAMe”).
• SAMe S-adenosyl-L-methionine
• the present invention is directed to the use of a combination of Lotus extract and methyl donors in oral and topical formulations. It is theorized that this combination may act in concert with or perhaps synergistically with one or more of the following ingredients:
• Vitamins are any of a group of organic substances essential in small quantities to normal metabolism. Synthetic vitamins are also available and may be utilized in the present invention. It is believed that the addition of one or more vitamins to the proposed combination would benefit the end user by providing components that may be needed in the cell repair process.
• Vitamin A is a fat soluble vitamin. Vitamin A has been demonstrated to aid bone development, strengthen the immune system and promote wound healing. Sources of Vitamin A include broccoli, cantaloupe, cod, halibut, kale, red peppers, spinach and watercress. The addition of natural or synthetic Vitamin A and derivatives thereof to the present invention would prove beneficial.
• Vitamin B-1 is a water soluble vitamin. Vitamin B-1 has been demonstrated to assist in the metabolism of proteins and fats. Sources of Vitamin B-1 include chick peas, pinto beans, soybeans, nuts, and salmon.
• Vitamin B-2 is a water soluble vitamin. Vitamin B-2 is essential for normal cell growth. Sources of Vitamin B-2 include almonds, walnuts and dairy products, such as cottage cheese, milk and yogurt. The addition of natural or synthetic Vitamin B-2 and derivatives thereof to the present invention would prove beneficial.
• Vitamin B-3 is a water-soluble vitamin. Vitamin B-3 has been demonstrated to protect against carcinogens and is useful in maintaining healthy skin. Sources of Vitamin B-3 include almonds, sunflower seeds, hazelnuts and yogurt.
• Vitamin B-6 is a water-soluble vitamin. Vitamin B-6 is essential for the proper functioning of over sixty enzymes. Sources of Vitamin B-6 include eggs, salmon, pinto beans and lentils.
• Vitamin B-12 is a water-soluble vitamin. Vitamin B12 helps maintain healthy cells. Sources of Vitamin B-12 include eggs, yogurt, salmon and halibut.
• Vitamin C or ascorbic acid, is one of several antioxidants shown to be essential for reducing free-radical induced cellular and molecular events when skin or cells are exposed to substantially high doses of ultraviolet B radiation. Vitamin C has also been shown to inhibit ultraviolet radiation-induced immunosuppression in vitro. Sources of Vitamin C include broccoli, cantaloupe, citrus, red peppers, strawberries and tomatoes.
• Vitamin D is a fat soluble vitamin. Vitamin D is essential in calcium absorption and metabolism. Sources of Vitamin D include fish, such as cod.
• Vitamin E is the ⁇ -form of tocopherol. There are four stereoisomers of tocopherol and four stereolsomers of tocotrienol. The tocopherols and the tocotrienols both contain a central aromatic chromanol nucleus and a 16-carbon member side chain. The side chain in the tocopherols is saturated. The side chain in the tocotrienols is not. Vitamin E is found in palm oil, soy bean oil, corn oil, canola oil, cranberry oil, rapeseed oil, rice bran oil, sunflower oil, safflower oil and cottonseed oil. However, of these, only cranberry oil, palm oil and rice bran oil contain tocotrienols.
• ⁇ -tocopherol is one of several antioxidants shown to be essential for reducing free-radical induced cellular and molecular events when skin or cells are exposed to substantially high doses of ultraviolet B radiation. ⁇ -tocopherol has also been shown to inhibit ultraviolet radiation-induced immunosuppression in vitro.
• Sources of Vitamin E include almonds, hazelnuts, pecans, sunflower seeds, asparagus, olives, and spinach.
• Vitamin F also known as Essential Fatty Acids or EFA, is a fat-soluble vitamin. Vitamin F consists of unsaturated fatty acids with two or more double bonds, such as linoleic acid and linolenic acid. The term Vitamin F was discredited by the American Medical Association in 1937. Sources of Vitamin F include vegetable oils, such as olive oil.
• Vitamin H also known as biotin, is a water soluble vitamin.
• Sources of biotin include liver, kidney, pancreas, yeast and milk.
• Vitamin K is a general term that refers to a group of naphthoquinone derivatives required for the bioactivation of proteins involved in blood coagulation or stagnation. Sources of Vitamin K include green plants and intestinal bacteria.
• any known minerals or their derivatives are useful in the present invention.
• minerals There are several definitions for minerals, including, “any substance that is neither animal nor vegetable.”
• the use of the term in the present invention is directed to any of a group of inorganic substances essential to the functioning of the human body and that are usually obtained from foods. It is believed that the addition of one or more minerals to the proposed combination would benefit the end user by providing components that may be needed in the cell repair process.
• Minerals useful in the present invention include copper, zinc, and manganese, for their role in forming the antioxidant, superoxide dismutase, and selenium and glutathione, for their role in function of glutathione peroxidase.
• Other minerals involved in cell function maintenance include calcium, magnesium and potassium.
• Other useful minerals include sulfur, chromium, iron, phosphorous and iodine.
• Antioxidants protect skin cells and collagen from free radical damage.
• the present invention combines Lotus and methyl donors with antioxidants to provide stronger damage protection.
• Some of the antioxidants useful in the present invention include glycyrrhiza glabra, quercetin, rosemary, sage, ginger, tumeric, carnosine, curcumin, limonene, silymarin, isoflavones, carotenoids, asaxanthin, lycopene, lutein, superoxide dismutase, aloe vera, carnosine, CoEnzyme Q10, hawthorne berry, hawthome berry extract, acerola, acerola extract, apricot, apricot extract, bilberry, bilberry extract, blackberry, blackberry extract, black currant, black currant extract, blueberry, blueberry extract, chaste berry, chaste berry extract, cherry, cherry extract, cranberry, cranberry extract, elderberry, elderberry
• Amino acids such as glycine, glutamine, proline, and lysine, are components of collagen and therefore useful in compositions of the present invention.
• Valine, arginine, and alanine are vital to skin repair.
• Collagen is one part of connective tissue and the major component of the skin. 4-hydroxyproline is found mainly in collagen.
• Serine is a non-essential amino acid for human development.
• Hormones are vital to the skin's natural metabolism. With age, hormone levels decline in the body and the skin. Cell function declines as hormonal levels drop. It is known that estrogen and testosterone can restore some youthfulness to the skin's appearance. This invention encompasses these and other compounds with hormonal activity that rejuvenate the skin's youthful appearance.
• Some of the hormones useful in the present invention include estrogen and its components (estradiol, estriol and estrone), testosterone, pregnenolone, progesterone, melatonin, and DHEA.
• Phytoestrogens from plants are also useful in the present invention and include soy and its constituents, yam, polygonum cuspidatum, black cohosh, licorice, grapes/resveratrol, dongquai, red clover, and vitex agnus castus.
• EGF Epidermal Growth Factor
• FGF Fibroblast Growth Factor
• IGF Insulin-like Growth Factor
• the present invention may also include the following conventional ingredients:
• ⁇ -hydroxy acids also known as fruit acids, are well-known skin rejuvenating agents for photoaged and aged skin.
• Some examples of ⁇ -hydroxy acids include citric, glycolic (sugar cane extract) and lactic acids.
• Glycerin is a common humectant in both topical and oral formulations. It is used to dissolve non-water soluble substances. It is also used to provide a moisture barrier between the skin and the environment.
• Rice bran oil walnut oil, almond oil, pumpkin seed oil, sunflower seed oil, safflower seed oil, fish oil, omega 3 fatty acids, omega 6 fatty acids, DNA/RNA, vitamin D, policosanol,
• surfactant is used to describe an additional group of additives to the present invention.
• Surfactants are solubilizers which are used to promote solubility.
• Surfactants for use in the present invention are pharmaceutically acceptable and include polysorbates and partial esters of common fatty acids, to name two of many available.
• Sunscreen agents are also within the scope of the present invention. Titanium dioxide is a well-known cosmetic ingredient used topically to protect the skin from photo-aging. Octylmethoxycinnamate, benzophenone, octylsalicylate, and parsol 1789 can also be used in combination with Lotus and/or methyl donors to increase the skin's defense against sun damage.
• topical or oral compositions of the present invention may be used at any appropriate daily intervals, depending of course upon the particular type of composition formulated.
• the Firming Antioxidant Serum as set forth in Example 2 hereinafter, is to be used anytime when desired, i.e., at night, under make-up, by itself, or before using or with other preparations.
• anyone skilled in the art obviously can formulate a myriad of products for special needs that would be within the scope of this invention.
• a composition according to the present invention may be in any of the cosmetic, pharmaceutical or dietary forms which are generally used for topical application such as liquids (both aqueous and non-aqueous solutions), creams (both oil-in-water and water-in-oil, O/W & W/O, emulsions), gels (both aqueous and non-aqueous), lotions, serums, ointments, paste, powders, liposomes, laminates, microspheres, capsules, and tablets.
• liquids both aqueous and non-aqueous solutions
• creams both oil-in-water and water-in-oil, O/W & W/O, emulsions
• gels both aqueous and non-aqueous
• lotions both aqueous and non-aqueous solutions
• serums both oil-in-water and water-in-oil, O/W & W/O, emulsions
• gels both aqueous and non-aqueous
• compositions of the present invention may also contain additives such as water, alcohols, oils (mineral vegetable, animal and synthetics), glycols, colorants, preservatives, emulsifiers, gelling agents, gums, esters, silicones, polymers, fragrances, flavors, active ingredients, acids, bases, buffers, salts, polyols, proteins and their derivatives, essential oils, tonics, waxes, lipids, stabilizers, fillers, celluloses, glycans, amines, solubilizers, thickeners, sugars and sugar derivatives, ceramides, sweeteners and the like, so long as such additives do not defeat the objectives of the present invention.
• additives such as water, alcohols, oils (mineral vegetable, animal and synthetics), glycols, colorants, preservatives, emulsifiers, gelling agents, gums, esters, silicones, polymers, fragrances, flavors, active ingredients, acids, bases, buffers, salts, polyols,
• moisturizers also appear to benefit the present invention in holding moisture in the skin, enhancing its repair process, protecting the skin barrier function and making the skin appear younger.
• a unique blend of protective antioxidants and essential nutrients with the entire Sacred Lotus seed in food preparations the pithe (embryo) or lumule is removed due to bitter taste) used to promote good health and radiant skin is provided.
• This product may be taken, for example, twice per day.
• the ingredients are mixed together using standard mixing techniques. A pleasant cream results.
• the ingredients are mixed together using standard mixing techniques. A pleasant serum results.
• the ingredients are mixed together using standard mixing techniques.
• the ingredients are mixed together using standard mixing techniques.

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• 2003
  • 2003-10-03 EP EP03759697A patent/EP1667699B1/de not_active Expired - Lifetime
  • 2003-10-03 WO PCT/US2003/031392 patent/WO2005041996A1/en active Application Filing
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  • 2003-10-03 US US10/573,933 patent/US20070116696A1/en not_active Abandoned
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